Preparing Phytosome Curcumin and PEG-CUR Complex

Abstract

Despite curcumin’s numerous pharmacological effects, it has been limitedly used in clinical practice due its low bioavailability. In this study, phytosome curcumin and PEG-CUR complex were prepared to increase their bioavailability. Phytosome curcumin was prepared by reaction between curcumin and phosphatidylcholine; PEG-CUR was prepared by reaction between curcumin and PEG. Phytosome curcumin and PEG-CUR were characterized by ¹H NMR, FTIR and DSC analysis. The physicochemical parameters such as zeta potential, size distribution, solubility and curcumin content were also investigated. The amount of curcumin in phytosome curcumin was 25.71 ± 0.46 % and in PEG-CUR was 13.26 ± 1.25 %. Phytosome curcumin has the size of 131.8 nm and the zeta potential of -48.4 mV, while PEG-CUR has the size of 96.3 nm and the zeta potential of -44.5 mV. The solubility of phytosome curcumin and PEG-CUR in certain media was higher than that of free curcumin. The in vivo assay showed that phytosome curcumin had stronger hepatoprotective effect in comparison with free curcumin. The administration of phytosome curcumin effectively suppressed paracetamol-induced liver injury evidenced by a reduction in lipid peroxidation level, and elevated enzymatic antioxidant activities of superoxide dismutase, catalase, and glutathione peroxidase in mice liver tissues. The study results also show that the cytotoxicity effect of PEG-CUR was much greater than that of free curcumin in HepG2 and HCT116 cancer cell lines.

Keywords

Curcumin, phytosome, PEGylation, solubility, cytotoxicity, hepatoprotective.

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